Assay Detail
Binding
CHEMBL798016
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Binding affinity against RXR alpha receptor using [3H]9-cis-RA as radioligand in CV-1 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Cell Type | CV-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.28 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL133915 | — | — | 1 | 9.10 |
| CHEMBL130374 | — | — | 1 | 9.10 |
| CHEMBL130232 | — | — | 1 | 9.00 |
| CHEMBL42314 | — | — | 1 | 8.82 |
| CHEMBL422088 | — | — | 1 | 8.64 |
| CHEMBL337393 | — | — | 1 | 8.59 |
| CHEMBL130317 | — | — | 1 | 8.52 |
| CHEMBL335242 | — | — | 1 | 8.39 |
| CHEMBL131826 | — | — | 1 | 8.36 |
| CHEMBL424639 | — | — | 1 | 8.21 |
| CHEMBL133896 | — | — | 1 | 8.20 |
| CHEMBL111217 | — | — | 1 | 8.11 |
| CHEMBL288436 | — | — | 1 | 7.89 |
| CHEMBL424269 | — | — | 1 | 7.67 |
| CHEMBL132568 | — | — | 1 | 7.59 |
| CHEMBL130231 | — | — | 1 | 7.54 |
| CHEMBL131122 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL133915 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL130374 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL130232 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL42314 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL422088 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL337393 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL130317 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL335242 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL131826 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL424639 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL133896 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL111217 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL288436 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL424269 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL132568 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL130231 | — | Ki | = | 28.7 | nM | 7.54 |
| CHEMBL131122 | — | Ki | = | 85.8 | nM | 7.07 |